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Development of sustained release formulation by using crystal transition of active ingredient.

Research Project

Project/Area Number 26460039
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Physical pharmacy
Research InstitutionUniversity of Shizuoka

Principal Investigator

Itai Shigeru  静岡県立大学, 薬学部, 教授 (80453059)

Co-Investigator(Kenkyū-buntansha) 岩尾 康範  静岡県立大学, 薬学部, 准教授 (30433022)
野口 修治  東邦大学, 薬学部, 教授 (60237823)
Project Period (FY) 2014-04-01 – 2017-03-31
Project Status Completed (Fiscal Year 2016)
Budget Amount *help
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2016: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2015: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2014: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Keywordssustained release / gastro-floating / Clarithromycin / polymorphism / クラリスロマイシン / 結晶転移 / 胃内滞留製剤 / 製造コスト削減 / 胃内浮遊性製剤 / ヘリコバクタピロリ除菌 / 溶融造粒 / 高薬物含有微粒子 / 放射光X線CT / 放出制御製剤
Outline of Final Research Achievements

Clarithromycin(CAM) has 2 crystal forms at ambient temperature and meta-stable crystal(FormⅠ) transforms to stable crystal(FormⅡ) and hydrate(FormⅣ) immediately by contact with water. By using this property, we succeeded in development of highly --loaded CAM sustained release formulation with 0-order manner and gastro-floating formulation. FormⅡ can be obtained by dispersion in water-filtration-drying processes or heat treatment(150℃). Since these treatment lead to increase API cost, we tried and establish the transformation of FormⅠto FromⅡ during the manufacturing process of CAM formulation.

Report

(4 results)
  • 2016 Annual Research Report   Final Research Report ( PDF )
  • 2015 Research-status Report
  • 2014 Research-status Report
  • Research Products

    (30 results)

All 2017 2016 2015 2014 Other

All Journal Article (15 results) (of which Int'l Joint Research: 2 results,  Peer Reviewed: 15 results,  Acknowledgement Compliant: 11 results,  Open Access: 2 results) Presentation (14 results) Remarks (1 results)

  • [Journal Article] Effect of gel formation on the dissolution behavior of clarithromycin tablets.2017

    • Author(s)
      Inukai K, Takiyama K, Noguchi S, Iwao Y, Itai S
    • Journal Title

      International Journal of Pharmaceutics

      Volume: 521 Issue: 1-2 Pages: 33-39

    • DOI

      10.1016/j.ijpharm.2017.01.065

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Enhancing the Solubility and Oral Bioavailability of Poorly Water-Soluble Drugs Using Monoolein Cubosomes2017

    • Author(s)
      Ali MA, Kataoka N, Ranneh AH, Iwao Y, Noguchi S, Oka T, Itai S.
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 65 Issue: 1 Pages: 42-48

    • DOI

      10.1248/cpb.c16-00513

    • NAID

      130005187634

    • ISSN
      0009-2363, 1347-5223
    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research / Acknowledgement Compliant
  • [Journal Article] Saturated fatty acids and fatty acid esters promote the polymorphic transition of clarithromycin metastable form I crystal.2016

    • Author(s)
      Watanabe M, Mizoguchi M, Aoki H, Iwao Y, Noguchi S, Itai S.
    • Journal Title

      International Journal of Pharmaceutics

      Volume: 512 Issue: 1 Pages: 108-117

    • DOI

      10.1016/j.ijpharm.2016.08.041

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Sustained-release microsphere formulation containing an agrochemical by polyurethane polymerization during an agitation granulation process.2016

    • Author(s)
      Terada T, Tagami M, Ohtsubo T, Iwao Y, Noguchi S, Itai S.
    • Journal Title

      International Journal of Pharmaceutics

      Volume: 509 Issue: 1-2 Pages: 328-337

    • DOI

      10.1016/j.ijpharm.2016.05.061

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Preparation and Characterization of SN-38-Encapsulated Phytantriol Cubosomes Containing α-Monoglyceride Additives2016

    • Author(s)
      Ali MA, Noguchi S, Iwao Y, Oka T, Itai S
    • Journal Title

      Chemical and Pharmaceutical Bulletin

      Volume: 64 Issue: 6 Pages: 577-584

    • DOI

      10.1248/cpb.c15-00984

    • NAID

      130005154404

    • ISSN
      0009-2363, 1347-5223
    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Open Access / Int'l Joint Research / Acknowledgement Compliant
  • [Journal Article] Clarithromycin highly-loaded gastro-floating fine granules prepared by high-shear melt granulation can enhance the efficacy of Helicobacter pylori eradication2015

    • Author(s)
      Aoki, H., Iwao, Y., Mizoguchi, M., Noguchi, S., Itai, S
    • Journal Title

      European Journal of Pharmaceutics and Biopharmaceutics

      Volume: 92 Pages: 22-27

    • DOI

      10.1016/j.ejpb.2015.02.012

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Suppressed release of clarithromycin from tablets by crystalline phase transition of metastable polymorph form I2015

    • Author(s)
      Fujiki, S., Watanabe, N., Iwao, Y., Noguchi, S., Mizoguchi, M., Iwamura, T., Itai, S.
    • Journal Title

      Journal of Pharmaceutical Sciences

      Volume: 104 Issue: 8 Pages: 2541-2644

    • DOI

      10.1002/jps.24516

    • Related Report
      2015 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Effect of surfactants or a water soluble polymer on the crystal transition of clarithromycin during a wet granulation process2015

    • Author(s)
      Nozawa, K., Iwao, Y., Noguchi, S., Itai, S
    • Journal Title

      International Journal of Pharmaceutics

      Volume: 495 Issue: 1 Pages: 204-217

    • DOI

      10.1016/j.ijpharm.2015.08.080

    • Related Report
      2015 Research-status Report
    • Peer Reviewed
  • [Journal Article] Polymorphic transformation of antibiotic clarithromycin under acidic condition2014

    • Author(s)
      Noguchi, S., Takiyama, K., Fujiki, S., Iwao, Y., Miura, K., Itai, S.
    • Journal Title

      Journal of Pharmaceutical Sciences,

      Volume: 103 Pages: 580-586

    • Related Report
      2014 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Evaluation of the physicochemical properties of fine globular granules prepared by a multi-functional rotor processor2014

    • Author(s)
      Kimura, S., Iwao, Y., Ishida, M., Noguchi, S., Itai, S., Uchida, S., Yamada, M., Namiki, N.
    • Journal Title

      Chemical & Pharmaceutical Bulletin

      Volume: 62 Pages: 1-7

    • NAID

      130003390776

    • Related Report
      2014 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Effects of the centrifugal coating and centrifugal fluidized bed coating methods on the physicochemical properties of sustained-release microparticles using a multi-functional rotor processor2014

    • Author(s)
      Yamada, N., Mise, R., Ishida, M., Iwao, Y., Noguchi, S., Itai, S.
    • Journal Title

      Advanced Powder Technology

      Volume: 25 Pages: 430-435

    • Related Report
      2014 Research-status Report
    • Peer Reviewed
  • [Journal Article] Development and evaluation of a tacrolimus cream formulation using a binary solvent system2014

    • Author(s)
      Yamanaka, M., Yokota, S., Iwao, Y., Noguchi S., Itai, S.
    • Journal Title

      International Journal of Pharmaceutics

      Volume: 464 Pages: 19-26

    • Related Report
      2014 Research-status Report
    • Peer Reviewed
  • [Journal Article] Development of highly stable nifedipine solid-lipid nanoparticles2014

    • Author(s)
      Barman, RK., Iwao, Y., Funakoshi, Y., Ranneh, AH., Noguchi S., Wahed, MII., Itai, S.
    • Journal Title

      Chemical & Pharmaceutical Bulletin

      Volume: 62 Pages: 1-8

    • NAID

      130004053796

    • Related Report
      2014 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] In vivo pharmacokinetic and hemocompatible evaluation of lyophilization induced nifedipine solid-lipid nanoparticle2014

    • Author(s)
      Barman, RK., Iwao, Y., Islam, Md., Funakoshi, Y., Noguchi S., Wahed, MII., Itai, S
    • Journal Title

      Pharmacology & Pharmacy

      Volume: 5 Pages: 455-461

    • Related Report
      2014 Research-status Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Impact of active ingredients on the swelling properties of orally disintegrating tablets prepared by microwave treatment2014

    • Author(s)
      Sano, S., Iwao, Y., Noguchi S., Kimura, S., Itai, S.
    • Journal Title

      International Journal of Pharmaceutics

      Volume: 468 Pages: 234-242

    • Related Report
      2014 Research-status Report
    • Peer Reviewed
  • [Presentation] 親水性高分子を用いたクラリスロマイシン準安定形結晶含有造粒物の調製2017

    • Author(s)
      渡邉美笛、岩尾康範、野口修治、木村晋一郎、板井茂
    • Organizer
      日本薬剤学会第32年会
    • Place of Presentation
      大宮
    • Year and Date
      2017-05-13
    • Related Report
      2016 Annual Research Report
  • [Presentation] cryo-TEM及びAFMによる脂質ナノ粒子の構造解析2017

    • Author(s)
      松尾聖羅、岩尾康範、東顕二郎、森部久仁一、木村晋一郎、板井茂
    • Organizer
      日本薬剤学会第32年会
    • Place of Presentation
      大宮
    • Year and Date
      2017-05-11
    • Related Report
      2016 Annual Research Report
  • [Presentation] 飽和脂肪酸や脂肪酸エステルが薬物の結晶転移に与える影響2016

    • Author(s)
      渡邉美笛、岩尾康範、野口修治、板井茂
    • Organizer
      日本病院薬剤師会東海ブロック・日本薬学会東海支部会 合同学術大会
    • Place of Presentation
      岐阜
    • Year and Date
      2016-10-30
    • Related Report
      2016 Annual Research Report
  • [Presentation] クラリスロマイシンのゲル化による溶出挙動への影響とゲル形成機構に関する研究2016

    • Author(s)
      犬飼晃基、瀧山圭、岩尾康範、野口修治、板井茂
    • Organizer
      日本薬剤学会第31年会
    • Place of Presentation
      岐阜
    • Year and Date
      2016-05-19
    • Related Report
      2016 Annual Research Report 2015 Research-status Report
  • [Presentation] Preparation and Characterization of SN-38-Encapsulated Phytantriol Cubosomes Containing α-Monoglyceride Additives2016

    • Author(s)
      アリ モハマド アシュラフ、岩尾康範、野口修治、岡俊彦、板井茂
    • Organizer
      日本薬剤学会第31年会
    • Place of Presentation
      岐阜
    • Year and Date
      2016-05-19
    • Related Report
      2016 Annual Research Report
  • [Presentation] クラリスロマイシン/脂質mixtureにおけるクラリスロマイシン結晶転移メカニズムの解明2016

    • Author(s)
      渡邉美笛
    • Organizer
      日本薬学会第136年会
    • Place of Presentation
      横浜」
    • Year and Date
      2016-03-28
    • Related Report
      2015 Research-status Report
  • [Presentation] カルボン酸塩によるクラリスロマイシンの放出抑制効果2015

    • Author(s)
      板井茂
    • Organizer
      日本薬剤学会第30年会
    • Place of Presentation
      長崎
    • Year and Date
      2015-05-21
    • Related Report
      2015 Research-status Report
  • [Presentation] クラリスロマイシンの除菌効果増強を目的とした薬物高含有胃内浮遊性粒子の設計と評価2014

    • Author(s)
      溝口緑理、青木肇、岩尾康範、野口修治、板井茂
    • Organizer
      日本病院薬剤師会東海ブロック・日本薬学会東海支部 合同学術大会
    • Place of Presentation
      静岡
    • Year and Date
      2014-11-09
    • Related Report
      2014 Research-status Report
  • [Presentation] Preparation and Evaluation of Gastro-Floating Fine Granules Prepared by Melt Granulation and Highly Loaded with Clarithromycin for Helicobacter Pylori Eradication2014

    • Author(s)
      Hajime Aoki, Midori Mizoguchi, Yasunori Iwao, Shuji Noguchi, and Shigeru Itai.
    • Organizer
      2014 American Association of Pharmaceutical Scientists Annual Meeting and Exposition
    • Place of Presentation
      San Diego, USA
    • Year and Date
      2014-11-05
    • Related Report
      2014 Research-status Report
  • [Presentation] 撹拌溶融造粒法を用いたいクラリスロマイシン高含有胃内浮遊性微小粒子の設計と評価2014

    • Author(s)
      青木肇、溝口緑理、岩尾康範、野口修治、板井茂
    • Organizer
      製剤機械技術学会第24回大会
    • Place of Presentation
      名古屋
    • Year and Date
      2014-10-08
    • Related Report
      2014 Research-status Report
  • [Presentation] ヘリコバクター・ピロリ除菌を目的としたクラリスロマイシン高含有胃内浮遊性粒子の設計と評価2014

    • Author(s)
      青木肇、溝口緑理、岩尾康範、野口修治、板井茂
    • Organizer
      第 60 回 日本薬学会東海支部 総会・大会
    • Place of Presentation
      鈴鹿
    • Year and Date
      2014-07-05
    • Related Report
      2014 Research-status Report
  • [Presentation] 放射光X線CT法を用いたワックスマトリックス製剤の溶出機構の解析2014

    • Author(s)
      岩本翔、野口修治、岩尾康範、板井茂
    • Organizer
      日本薬剤学会第29年会
    • Place of Presentation
      大宮
    • Year and Date
      2014-05-20
    • Related Report
      2014 Research-status Report
  • [Presentation] 放射光X線CT法を用いた錠剤内部構造解析2014

    • Author(s)
      梶原隆介、野口修治、岩尾康範、鈴木芳夫、寺田靖子、上杉健太朗、板井茂
    • Organizer
      日本薬剤学会第29年会
    • Place of Presentation
      大宮
    • Year and Date
      2014-05-20
    • Related Report
      2014 Research-status Report
  • [Presentation] 撹拌溶融造粒法によるクラリスロマイシン高含有胃内浮遊性粒子の設計と評価2014

    • Author(s)
      青木肇、岩尾康範、野口修治、板井茂
    • Organizer
      日本薬剤学会第29年会
    • Place of Presentation
      大宮
    • Year and Date
      2014-05-20
    • Related Report
      2014 Research-status Report
  • [Remarks] 静岡県立大学薬学部 創剤科学分野 創剤工学研究室

    • URL

      http://w3pharm.u-shizuoka-ken.ac.jp/pharmeng/

    • Related Report
      2016 Annual Research Report

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Published: 2014-04-04   Modified: 2018-03-22  

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